Title : Potency, voltage-dependency, agonist concentration-dependency, blocking kinetics and partial untrapping of the uncompetitive N-methyl-D-aspartate (NMDA) channel blocker memantine at human NMDA (GluN1/GluN2A) receptors.

Pub. Date : 2009 Apr

PMID : 19371579






2 Functional Relationships(s)
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1 In the present study we compared the potency of memantine, ketamine and (+)MK-801 in binding to NMDA receptors in post-mortem human cortical tissue and to antagonize intracellular Ca(2+) responses of human GluN1/GluN2A receptors expressed in HEK-293 cells. Memantine glutamate ionotropic receptor NMDA type subunit 2A Homo sapiens
2 Memantine was confirmed to be a moderate affinity (IC(50) at -70 mV of 0.79+/-0.02 microM, Hill=0.92+/-0.02), strongly voltage-dependent (delta=0.90+/-0.09) uncompetitive antagonist of human GluN1/GluN2A receptors. Memantine glutamate ionotropic receptor NMDA type subunit 2A Homo sapiens